KR102004059B1 - 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형 - Google Patents

6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형 Download PDF

Info

Publication number
KR102004059B1
KR102004059B1 KR1020177006011A KR20177006011A KR102004059B1 KR 102004059 B1 KR102004059 B1 KR 102004059B1 KR 1020177006011 A KR1020177006011 A KR 1020177006011A KR 20177006011 A KR20177006011 A KR 20177006011A KR 102004059 B1 KR102004059 B1 KR 102004059B1
Authority
KR
South Korea
Prior art keywords
crystalline form
peak
benzoxazole
crystalline
dichlorophenyl
Prior art date
Application number
KR1020177006011A
Other languages
English (en)
Korean (ko)
Other versions
KR20170040314A (ko
Inventor
케빈 폴 지라드
앤드류 제이. 젠센
크리스 니콜 존스
Original Assignee
화이자 인코포레이티드
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54199901&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR102004059(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 화이자 인코포레이티드 filed Critical 화이자 인코포레이티드
Publication of KR20170040314A publication Critical patent/KR20170040314A/ko
Application granted granted Critical
Publication of KR102004059B1 publication Critical patent/KR102004059B1/ko

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57Aryl or substituted aryl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
KR1020177006011A 2014-09-08 2015-08-31 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형 KR102004059B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462047614P 2014-09-08 2014-09-08
US62/047,614 2014-09-08
US201562203953P 2015-08-12 2015-08-12
US62/203,953 2015-08-12
PCT/IB2015/056597 WO2016038500A1 (en) 2014-09-08 2015-08-31 Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole

Publications (2)

Publication Number Publication Date
KR20170040314A KR20170040314A (ko) 2017-04-12
KR102004059B1 true KR102004059B1 (ko) 2019-07-25

Family

ID=54199901

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177006011A KR102004059B1 (ko) 2014-09-08 2015-08-31 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형

Country Status (24)

Country Link
US (1) US9770441B1 (lt)
EP (3) EP3977993B1 (lt)
JP (4) JP2016065042A (lt)
KR (1) KR102004059B1 (lt)
CN (2) CN106715405A (lt)
AU (1) AU2015313875B2 (lt)
BR (1) BR112017003421B1 (lt)
CA (1) CA2903194A1 (lt)
CY (1) CY1124843T1 (lt)
DK (1) DK3977993T3 (lt)
ES (2) ES2975633T3 (lt)
FI (1) FI3977993T3 (lt)
HR (1) HRP20211834T1 (lt)
HU (2) HUE065233T2 (lt)
IL (1) IL251037B1 (lt)
LT (1) LT3191461T (lt)
MX (1) MX2017002954A (lt)
PL (2) PL3977993T3 (lt)
PT (2) PT3977993T (lt)
RS (1) RS62634B1 (lt)
SG (1) SG11201700958YA (lt)
SI (2) SI3977993T1 (lt)
TW (1) TWI644902B (lt)
WO (1) WO2016038500A1 (lt)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2571950A (en) * 2018-03-13 2019-09-18 Azad Pharma Ag New polymorph and new path to synthesize tafamidis
WO2020128816A2 (en) 2018-12-20 2020-06-25 Pfizer Inc. Pharmaceutical compositions and methods comprising a combination of a benzoxazole transthyretin stabilizer and an additional therapeutic agent
CN113874359B (zh) * 2019-04-11 2024-07-16 Inke股份公司 用于制备1-脱氧-1-甲基氨基-d-葡萄糖醇2-(3,5-二氯苯基)-6-苯并𫫇唑羧酸盐的方法
US20220259162A1 (en) * 2019-05-16 2022-08-18 Teva Pharmaceuticals International Gmbh Solid state forms of tafamidis and salts thereof
US20220251052A1 (en) * 2019-07-04 2022-08-11 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid or its pharmaceutically acceptable salts and polymorphs thereof
WO2021093809A1 (zh) 2019-11-15 2021-05-20 苏州科睿思制药有限公司 他发米帝司的晶型及其制备方法和用途
CA3165298A1 (en) * 2019-12-20 2021-06-24 Pfizer Ireland Pharmaceuticals Efficient process for making 6-carboxy benzoxazole derivatives
WO2021152623A1 (en) * 2020-01-27 2021-08-05 Dr. Reddy’S Laboratories Limited Improved processes for the preparation of tafamidis and its meglumine salt
WO2021232619A1 (zh) * 2020-05-19 2021-11-25 苏州科睿思制药有限公司 一种他发米帝司游离酸的晶型及其制备方法和用途
US20230265059A1 (en) * 2020-07-04 2023-08-24 Nuray Chemicals Private Limited Solid state forms of 6-carboxy-2-(3, 5-dichlorophenyl)-benzoxazole of formula-i and pharmaceutically acceptable salts thereof
WO2022084790A1 (en) * 2020-10-19 2022-04-28 Glenmark Life Sciences Limited Process for preparation of tafamidis and salts thereof
WO2022107166A1 (en) * 2020-11-20 2022-05-27 Natco Pharma Limited Novel crystalline form of tafamidis and its process thereof
WO2022112919A1 (en) 2020-11-25 2022-06-02 Pfizer Inc. (aza)benzothiazolyl substituted pyrazole compounds
CN114907283A (zh) * 2021-02-07 2022-08-16 南京正大天晴制药有限公司 一种2-(3,5-二氯苯基)-苯并噁唑-6-羧酸的制备方法
EP4083027A1 (en) 2021-04-26 2022-11-02 Química Sintética, S.A. A solid state form of tafamidis and a process for its preparation
WO2023020762A1 (en) 2021-08-16 2023-02-23 Synthon B.V. Crystalline forms of tafamidis nicotinamide adduct
WO2023091534A1 (en) 2021-11-17 2023-05-25 Teva Pharmaceuticals International Gmbh Solid state form of tafamidis
WO2024023710A1 (en) 2022-07-28 2024-02-01 Pfizer Inc. Tafamidis pharmaceutical compositions
WO2024084362A1 (en) * 2022-10-17 2024-04-25 Biophore India Pharmaceuticals Pvt. Ltd A process for the preparation of crystalline form of tafamidis
US11878081B1 (en) 2022-12-23 2024-01-23 Tap Pharmaceuticals Ag Pharmaceutical formulations of tafamidis
US11980685B1 (en) 2022-12-23 2024-05-14 Tap Pharmaceuticals, Ag Liquid pharmaceutical formulations of tafamidis

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7214695B2 (en) * 2002-12-19 2007-05-08 The Scripps Research Institute Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
WO2013038351A1 (en) * 2011-09-16 2013-03-21 Pfizer Inc. Solid forms of a transthyretin dissociation inhibitor

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
CN103923169B (zh) * 2006-12-06 2017-05-24 科内图斯医药公司 (3s)‑3‑[n‑(n’‑(2‑叔丁基苯基)草氨酰基)丙氨酰基]氨基‑5‑(2’,3’,5’,6’‑四氟苯氧基)‑4‑氧代戊酸的结晶形式
US8576985B2 (en) 2009-09-01 2013-11-05 Aptuit (West Lafayette) Llc Methods for indexing solid forms of compounds
US9499527B2 (en) * 2012-05-10 2016-11-22 Cellix Bio Private Limited Compositions and methods for the treatment of familial amyloid polyneuropathy
GB2571950A (en) 2018-03-13 2019-09-18 Azad Pharma Ag New polymorph and new path to synthesize tafamidis
US20220259162A1 (en) 2019-05-16 2022-08-18 Teva Pharmaceuticals International Gmbh Solid state forms of tafamidis and salts thereof
US20220251052A1 (en) 2019-07-04 2022-08-11 Msn Laboratories Private Limited, R&D Center Improved process for the preparation of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid or its pharmaceutically acceptable salts and polymorphs thereof
WO2021152623A1 (en) 2020-01-27 2021-08-05 Dr. Reddy’S Laboratories Limited Improved processes for the preparation of tafamidis and its meglumine salt

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7214695B2 (en) * 2002-12-19 2007-05-08 The Scripps Research Institute Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
WO2013038351A1 (en) * 2011-09-16 2013-03-21 Pfizer Inc. Solid forms of a transthyretin dissociation inhibitor

Also Published As

Publication number Publication date
AU2015313875A1 (en) 2017-03-02
DK3977993T3 (da) 2024-02-19
PL3191461T3 (pl) 2022-02-07
RS62634B1 (sr) 2021-12-31
SI3191461T1 (sl) 2022-01-31
AU2015313875B2 (en) 2018-03-15
CY1124843T1 (el) 2022-11-25
IL251037B1 (en) 2024-10-01
NZ766084A (en) 2023-12-22
JP2016065042A (ja) 2016-04-28
BR112017003421B1 (pt) 2023-10-10
PT3977993T (pt) 2024-04-01
RU2017107235A3 (lt) 2018-10-11
NZ729011A (en) 2023-10-27
ES2975633T3 (es) 2024-07-10
PL3977993T3 (pl) 2024-05-06
HRP20211834T1 (hr) 2022-03-04
SG11201700958YA (en) 2017-03-30
ES2901785T3 (es) 2022-03-23
JP2023134645A (ja) 2023-09-27
JP7357525B2 (ja) 2023-10-06
SI3977993T1 (sl) 2024-05-31
TW201613880A (en) 2016-04-16
EP4349406A2 (en) 2024-04-10
RU2692252C2 (ru) 2019-06-24
FI3977993T3 (fi) 2024-03-25
CA2903194A1 (en) 2016-03-08
JP2022024014A (ja) 2022-02-08
EP3977993B1 (en) 2024-01-31
IL251037A0 (en) 2017-04-30
US9770441B1 (en) 2017-09-26
HUE065233T2 (hu) 2024-05-28
EP3191461A1 (en) 2017-07-19
CN106715405A (zh) 2017-05-24
EP3191461B1 (en) 2021-11-03
HUE056583T2 (hu) 2022-02-28
KR20170040314A (ko) 2017-04-12
US20170273953A1 (en) 2017-09-28
MX2017002954A (es) 2017-06-15
RU2017107235A (ru) 2018-10-11
EP4349406A3 (en) 2024-05-22
WO2016038500A1 (en) 2016-03-17
CN115368313A (zh) 2022-11-22
TWI644902B (zh) 2018-12-21
JP2020055832A (ja) 2020-04-09
LT3191461T (lt) 2021-12-10
BR112017003421A2 (pt) 2017-11-28
PT3191461T (pt) 2021-12-27
EP3977993A1 (en) 2022-04-06

Similar Documents

Publication Publication Date Title
KR102004059B1 (ko) 6-카르복시-2-(3,5-디클로로페닐)-벤족사졸의 고체 결정형
US9249112B2 (en) Solid forms of a transthyretin dissociation inhibitor
EP4352051A1 (en) New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide
NZ729011B2 (en) Crystalline solid forms of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole
EA027972B1 (ru) Новая кристаллическая форма
NZ621194B2 (en) Solid forms of a transthyretin dissociation inhibitor
KR20210135530A (ko) Flna-결합 화합물 및 이의 하이드로클로라이드 염의 고체 다형체

Legal Events

Date Code Title Description
A201 Request for examination
AMND Amendment
E902 Notification of reason for refusal
AMND Amendment
E601 Decision to refuse application
AMND Amendment
X701 Decision to grant (after re-examination)